The oral bioavailability of BCS (biopharmaceutics classification system) class II drugs with poor solubility and reasonable permeability is limited by the drug dissolution step from drug products. Though prodrug approach is an exciting way of improving the oral bioavailability, it requires extensive studies to establish the safety profile of prodrugs in humans. In view of the increasing market share of oral drug products, a variety of technologies are developed to enhance the oral bioavailability of poorly soluble drugs using the excipients with approved or GRAS (generally regarded as safe) status. The present review describes the main technologies such as micronization, nanosizing, crystal engineering, solid dispersions, cyclodextrins, solid lipid nanoparticles and other colloidal drug delivery systems with a few relevant research reports.
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